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<p>Mutant IDH1 plays a significant role in cancers like gliomas and AML by producing the harmful metabolite D-2HG, which disrupts cell function. Over the years, researchers have developed selective inhibitors such as Ivosidenib, Vorasidenib, and Olutasidenib, improving potency, stability, and blood–brain barrier penetration. Structural modifications have significantly enhanced drug effectiveness, including fluorinated groups and diverse heterocyclic compounds like triazine, pyrazole, and quinoline. Advanced synthesis methods like palladium-catalyzed coupling and nucleophilic substitution have further refined these inhibitors. This review addresses a thorough analysis of synthetic methodologies, SAR optimizations, and pharmacokinetics of the reported inhibitors of mIDH1.</p>

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Scaffold modification and synthesis routes for targeting mutant IDH 1: a review

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2025年7月1日

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  • Vasavi S. Pai,
  • N. V. Anil Kumar

摘要

Mutant IDH1 plays a significant role in cancers like gliomas and AML by producing the harmful metabolite D-2HG, which disrupts cell function. Over the years, researchers have developed selective inhibitors such as Ivosidenib, Vorasidenib, and Olutasidenib, improving potency, stability, and blood–brain barrier penetration. Structural modifications have significantly enhanced drug effectiveness, including fluorinated groups and diverse heterocyclic compounds like triazine, pyrazole, and quinoline. Advanced synthesis methods like palladium-catalyzed coupling and nucleophilic substitution have further refined these inhibitors. This review addresses a thorough analysis of synthetic methodologies, SAR optimizations, and pharmacokinetics of the reported inhibitors of mIDH1.